US6146841AExpiredUtility

Methods for identifying compounds that bind to CSAPK-3 molecules and fragments thereof

38
Assignee: MILLENNIUM PHARM INCPriority: Sep 9, 1998Filed: Dec 28, 1998Granted: Nov 14, 2000
Est. expirySep 9, 2018(expired)· nominal 20-yr term from priority
Inventors:Susan Acton
G01N 33/5005A01K 2217/05A61N 1/3655C07K 2319/00C12N 9/1205C12Q 1/48C12Q 1/485G01N 33/5008G01N 33/5014G01N 33/502G01N 33/68G01N 33/6893G01N 2500/00G01N 2800/32
38
PatentIndex Score
2
Cited by
48
References
64
Claims

Abstract

The present invention provides methods for identifying compounds that bind to CSAPK-3, a cardiovascular system associated protein kinase.

Claims

exact text as granted — not AI-modified
What is claimed: 
     
       1. A method for identifying a compound which modulates the binding or kinase activity of a polypeptide comprising the amino acid sequence of SEQ ID NO:8, the method comprising: a) contecting a cell expressing the polypeptide with a rest compound under conditions suitable for modulation of the binding or kinase activity of the polypeptide; and   b) detecting modulation of the binding or kinase activity of the polypeptide by the test compound.   
     
     
       2. A method for identifying a compound which modulates the binding or kinase activity of a polypeptide consisting of the amino acid sequence of SEQ ID NO:8; the method comprising: a) contacting a cell expressing the polypeptide with a test compound under conditions suitable for modulation of the binding or kinase activity of the polypeptide; and   b) detecting modulation of the activity of the binding or kinase polypeptide by the test compound.   
     
     
       3. A method for identifying a compound which modulates the binding or kinase activity of a naturally occurring allelic variant of apolypeptide consisting of the amino acid sequence of SEQ ID NO:8, wherein the allelic variant is encoded by a nucleic acid molecule which hybridizes to the complement of a nucleic acid molecule consisting of SEQ ID NO:7 or 9, in 6×SSC at 45° C., followed by one or more washes in 0.2×SSC, 0.1% SDS at 50-65° C., the method comprising: a) contacting a cell expressing the allelic variant with a test compound under conditions suitable for modulation of the binding or kinase activity of the allelic variant; and   b) detecting modulation of the binding or kinase activity of the allelic variant by the test compound.   
     
     
       4. A method for identifying a compound which modulates the kinase activity of a polypeptide comprising at least 100 coniguous amino acids of SEQ ID NO:8, the method comprising: a) contacting a cell expressing the polypeptide with a test compound under conditions suitable for modulation of the kinase activity of the polypeptide; and   b) detecting modulation of the kinase activity of the polypeptide by the test compound.   
     
     
       5. The method of claim 1, wherein said modulation of the activity of the polypeptide is detected by direct binding of the test compound to the polypeptide. 
     
     
       6. The method of claim 5, wherein said direct binding is determined by lysing the cell and performing an immunoprecipitation. 
     
     
       7. The method of claim 5, wherein said direct binding is determined by a yeast two-hybrid assay. 
     
     
       8. The method of claim 1, wherein said modulation of the activity of the polypeptide is detected by use of an assay for CSAPK-1 activity. 
     
     
       9. The method of claim 1, wherein said cell expressing said polypeptide is a heart cell. 
     
     
       10. A method for identifying a compound which modulates the binding or kinase activity of a polypeptide comprising the amino acid sequence of SEQ ID NO:8, the method comprising: a) contacting the polypeptide with a test compound under conditions suitable for modulation of the binding or kinase activity of the polypeptide; and   b) detecting modulation of the binding or kinase activity of the polypeptide by the test compound.   
     
     
       11. A method for identifying a compound which modulates the binding or Kinase activity of a polypeptide consisting of the amino acid sequence of SEQ ID NO:8, the method comprising: a) contacting the polypeptide with a test compound under conditions suitable for modulation of the activity of the binding or kinase polypepride; and   b) detecting modulation of the activity of the binding or Kinase polypeptide by the test compound.   
     
     
       12. A method for identifying a compound which modulates the binding or kinase activity of a naturally occurring allelic variant of a polypeptide consisting of the amino acid sequence of SEQ ID NO:8, wherein the allelic variant is encoded by a nucleic acid molecule which hybridizes to the complement of a nucleic acid molecule consisting of SEQ ID NO:7 or 9, in 6×SSC at 45° C., followed by one or more washes in 0.2×SSC, 0.1% SDS at 50-65° C., the method comprising: a) contcting the allelic variant with a test compound under conditions suitable for modulation of the binding or kinase activity of the polypeptide; and   b) detecting modulation of the activity of the binding or kinase allelic variant by the test comapound.   
     
     
       13. A method for identifying a compound which modulates the kinase activity of a polypeptide comprising at least 100 contiguous amino acids of SEQ ID NO:8, the method comprising: a) contacting the polypeptide with a test compound under conditions suitable for modulation of the kinase activity of the polypeptide; and   b) detecting modulation of the kinase activity of the polypeptde by the test compound.   
     
     
       14. The method of claim 2, wherein said modulation of the activity of the polypeptide is detected by direct binding of the test compound to the polypepride. 
     
     
       15. The method of claim 14, wherein said direct binding is determined by lysing the cell and performing an immunoprecipitation. 
     
     
       16. The method of claim 14, wherein said direct binding is determined by a yeast two-hybrid assay. 
     
     
       17. The method of claim 3, wherein said modulation of the activity of the allelic variant is detected by direct binding of the test compound to the allelic variant. 
     
     
       18. The method of claim 17, wherein said direct binding is determined by lysing the cell and performing an immunoprecipitation. 
     
     
       19. The method of claim 17, wherein said direct binding is determined by a yeast two-hybrid assay. 
     
     
       20. The method of claim 4, wherein said modulation of the activity of the polypeptide is detected by direct binding of the test compound to the polypeptide. 
     
     
       21. The method of claim 20, wherein said direct binding is determined by lysing the cell and performing an immunoprecipitation. 
     
     
       22. The method of claim 20, wherein said direct binding is determined by a yeast two-hybrid assay. 
     
     
       23. The method of claim 10, wherein said modulation of the activity of the polypeptide is detected by direct binding of the test compound to the polypeptide. 
     
     
       24. The method of claim 23, wherein said direct binding is determined by an immunoprecipitation. 
     
     
       25. The method of claim 11, wherein said modulation of the activity of the polypeptide is detected by direct binding of the test compound to the polypeptide. 
     
     
       26. The method of claim 25, wherein said direct binding is determined by an immunoprecipitaiion. 
     
     
       27. The method of claim 12, wherein said modulation of the activity of the allelic variant is detected by direct binding of the test compound to the allelic variant. 
     
     
       28. The method of claim 27, wherein said direct binding is determined by an immunoprecipitition. 
     
     
       29. The method of claim 13, wherein said modulation of the activity of the polypeptide is detected by direct binding of the test compound to the polypeptide. 
     
     
       30. The method of claim 29, wherein said direct binding is determined by an immunoprecipition. 
     
     
       31. The method of claim 10, wherein said modulation of the activity of the polypeptide is detected by the use of a competition binding assay. 
     
     
       32. The method of claim 11, wherein said modulation of the activity of the polypeptide is detected by the use of a competition binding assay. 
     
     
       33. The method of claim 12, wherein said modulation of the activity of the allelic variant is detected by the use of a competition binding assay. 
     
     
       34. The method of claim 13, wherein said modulation of the activity of the polypeptide is detected by the use of a competition binding assay. 
     
     
       35. The method of claim 2, wherein said modulation of the activity of polypeptide is detected by use of an assay for CSAPK-3 activity. 
     
     
       36. The method of claim 3, wherein said modulation of the activity of the allelic variant is detected by use of an assay for CSAPK-3 activity. 
     
     
       37. The method of claim 4, wherein said modulation of the activity of the polypeptide is detected by use of an assay for CSAPK-3 activity. 
     
     
       38. The method of claim 10, wherein said modulation of the activity of the polypeptide is detected by use of an assay for CSAPK-3 activity. 
     
     
       39. The method of claim 38, wherein said assay for CSAPK-3 activity is based on the phosphorylation of a CSAPK-3 substrate. 
     
     
       40. The method of claim 11, wherein said modulation of the activity of the polypeptide is detected by use of an assay for CSAPK-3 activity. 
     
     
       41. The method of claim 40, wherein said assay for CSAPK-3 activity is based on the phosphorylation of a CSAPK-3 substrate. 
     
     
       42. The method of claim 12, wherein said modulation of the activity of the allelic variant is detected by use of an assay for CSAPK-3 activity. 
     
     
       43. The method of claim 42, wherein said assay for CSAPK-3 activity is based on the phosphorylation of a CSAPK-3 substrate. 
     
     
       44. The method of claim 13, wherein said modulation of the activity of the polypepride is detected by use of an assay for CSAPK-3 activity. 
     
     
       45. The method of claim 44, wherein said assay for CSAPK-3 activity is based on the phosphorylation of a CSAPK-3 substrate. 
     
     
       46. The method of claim 2, wherein said cell expressing said polypeptide is a heart cell. 
     
     
       47. The method of claim 3, wherein said cell expressing said allelic variant is a heart cell. 
     
     
       48. The method of claim 4, wherein said cell expressing said polypeptide is a heart cell. 
     
     
       49. The method of claim 1, wherein said modulation of the activity of the polypeptide is inhibition of the activity of the polypeptide. 
     
     
       50. The method of claim 2, wherein said modulation of the activity of the polypeptide is inhibition of the activity of the polypeptide. 
     
     
       51. The method of claim 3, wherein said modulation of the activity of the allelic variant is inhibition of the activity of the allelic variant. 
     
     
       52. The method of claim 4, wherein said modulation of the activity of the polypeptide is inhibition of the activity of the polypeptide. 
     
     
       53. The method of claim 10, wherein said modulation of the activity of the polypeptide is inhibition of the activity of the polypeptide. 
     
     
       54. The method of claim 11, wherein said modulation of the activity of the polypeptide is inhibition of the activity of the polypeptide. 
     
     
       55. The method of claim 12, wherein said modulation of the activity of the allelic variant is inhibition of the activity of the allelic variant. 
     
     
       56. The method of claim 13, wherein said modulation of the activity of the polypeptide is inhibition of the activity of the polypeptide. 
     
     
       57. The method of claim 1, wherein said modulation of the activity of the polypeptide is stimulation of the activity of the polypeptide. 
     
     
       58. The method of claim 2, wherein said modulation of the activity of the polypeptide is stimulation of the activity of the polypeptide. 
     
     
       59. The method of claim 3, wherein said modulation of the activity of the allelic variant is stimulation of the activity of the allelic variant. 
     
     
       60. The method of claim 4, wherein said modulation of the activity of the polypeptide is stimulation of the activity of the polypeptide. 
     
     
       61. The method of claim 10, wherein said modulation of the activity of the polypeptide is stimulation of the activity of the polypeptide. 
     
     
       62. The method of claim 11, wherein said modulation of the activity of the polypeptide is stimulation of the activity of the polypeptide. 
     
     
       63. The method of claim 12, wherein said modulation of the activity of the allelic variant is stimulation of the activity of the allelic variant. 
     
     
       64. The method of claim 13, wherein said modulation of the activity of the polypeptide is stimulation of the activity of the polypeptide.

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